Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof in which q, R11, R12, R13 and R14 are as defined in the specification, for use in therapy.

Abstract: This invention relates to triazolones and triazolones for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of triazolones in the treatment of cancer.

Abstract: Disclosed are a compound represented by Formula (1), or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, tautomer, enantiomer, or pharmaceutically acceptable diastereomer thereof, a method of preparing the same, and a pharmaceutical composition, which have effects for treatment or prevention of metabolic syndromes, comprising the same: wherein R1 to R6, X1 to X4, and n are the same as defined in Claim 1.

Abstract: The invention provides improved methods of synthesizing oltipraz, which result in higher overall yield and better purity of the desired product.

Abstract: A method of performing a chemical reaction includes reacting a compound selected from the group consisting of an organohalide and an organo-pseudohalide, and a protected organoboronic acid represented by formula (I) in a reaction mixture: R1—B-T ??(I); where R1 represents an organic group, T represents a conformationally rigid protecting group, and B represents boron having sp3 hybridization. When unprotected, the corresponding organoboronic acid is unstable by the boronic acid neat stability test. The reaction mixture further includes a base having a pKB of at least 1 and a palladium catalyst. The method further includes forming a cross-coupled product in the reaction mixture.

Abstract: This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I) wherein R1a, R1b, R2a, R2b, R3, R4a, R4b, and R5 are described herein.

Abstract: The invention relates to a compound of formula (I) wherein A and R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.

Abstract: The present invention includes compounds and compositions known to modify the perception of bitter taste, and combinations of said compositions and compounds with additional compositions, compounds, and products.

Abstract: The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract: The present invention relates to an improved synthesis of N-monofluoroalkyl tropanes using fluoroalkyl iodide. The invention also provides the use of such method to prepare the non-radioactive tropane intermediate FP-CIT, and its subsequent conversion to the 123I-labelled radiopharmaceutical DaTSCAN™ (123I-ioflupane). Also provided is the use of fluoroalkyl iodide in the alkylation method of the invention.

Abstract: Provided herein, inter alia, are methods and compositions for inhibiting ?v?1 integrin and for treating fibrosis.

Abstract: A compound represented by the general formula (I) or a pharmacologically acceptable salt thereof has an excellent LCAT-activating effect and is useful as an active ingredient in a therapeutic or prophylactic agent for arteriosclerosis, arteriosclerotic heart disease, coronary heart disease (including heart failure, myocardial infarction, angina pectoris, cardiac ischemia, cardiovascular disturbance, and restenosis caused by angiogenesis), cerebrovascular disease (including stroke and cerebral infarction), peripheral vascular disease (including diabetic vascular complications), dyslipidemia, hypo-HDL-cholesterolemia, hyper-LDL-cholesterolemia, or renal disease, particularly, an anti-arteriosclerotic agent, wherein R is an optionally substituted aryl group or an optionally substituted heteroaryl group, and R1 is a hydrogen atom or a hydroxy group.

Abstract: A series of fused tricyclic imidazole derivatives, in particular dihydro-1H-cyclopenta[4,5]imidazo[1,2-a]pyridine derivatives, and analogues thereof, being potent modulators of human TNF? activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.

Abstract: The present invention discloses salts of a Compound 1: useful in the prophylaxis and/or treatment of inflammatory conditions, autoimmune diseases, proliferative diseases, allergy, transplant rejection, diseases involving degradation and/or disruption of cartilage homeostasis, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons.

Abstract: The present invention is directed to a processes for the synthesis of 3-(3-(4-(1-aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine:

Abstract: The present invention is directed to compounds of Formulas (I, IIa and IIb): The invention also relates to pharmaceutical compositions comprising compounds of Formulas (I, IIa and IIb). Methods of making and using the compounds of Formulas (I, IIa and IIb) are also within the scope of the invention.

Abstract: The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.

Abstract: Disclosed is a compound represented by formula (I) or a pharmaceutically acceptable salt thereof as an inhibitor of phosphodiesterase type 5 and its therapeutic use in treating and/or preventing a disease or condition related with phosphodiesterase type 5 in a mammal wherein an inhibition of phosphodiesterase type 5 is considered beneficial

Abstract: Polymorphs of (S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one, compositions thereof, methods for their preparation, and methods for their use are disclosed.

Abstract: A series of substituted imidazo[1,2-b]pyridazine derivatives of formula (I), being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.

Abstract: A series of substituted imidazo[1,2-b][1,2,4]triazine derivatives of formula (I), being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.

Abstract: The present invention relates to heterocyclic compounds of the general formula (I) their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers, and polymorphs. The invention also relates to processes for the preparation of the compounds of invention, pharmaceutical compositions containing the compounds and their use as selective Bruton's Tyrosine Kinase (BTK) inhibitors.

Abstract: The present invention provides a compound of formula (1), wherein R1, R2, R3, R4a, R4b, R5a and R5b are as defined in the description, which has an autotaxin inhibitory activity, a pharmaceutical composition comprising the compound as an active ingredient, and a method of prevention or treatment of a disease involving autotaxin, which is characterized by administering the compound.

Abstract: Novel FXR agonists are disclosed, embodiments of a method of making the same, and of a composition comprising them are disclosed herein. Also disclosed are embodiments of a method of treating or preventing a metabolic disorder in a subject, comprising administering to a subject (e.g., via the gastrointestinal tract) a therapeutically effective amount of one or more of the disclosed compounds, thereby activating FXR receptors in the intestines, and treating or preventing a metabolic disorder in the subject. Additionally disclosed are embodiments of a method of treating or preventing inflammation in an intestinal region of a subject, comprising administering to the subject (e.g., via the gastrointestinal tract) a therapeutically effective amount of one or more of the disclosed compounds, thereby activating FXR receptors in the intestines, and thereby treating or preventing inflammation in the intestinal region of the subject.

Abstract: The present invention is directed to compounds of Formula I: wherein A is phenyl, naphthalenyl, pyridyl, quinolinyl, isoquinolinyl, imidazopyridyl, furanyl, thiazolyl, isoxazolyl, pyrazolyl, imidazothiazolyl, benzimidazolyl, or indazolyl; R1 is H, alkyl, alkoxy, hydroxyalkylene, OH, halo, phenyl, triazolyl, oxazolyl, isoxazolyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, piperazinyl, pyrazolyl, oxadiazolyl, pyrrolidinyl, thiophenyl, morpholinyl, or dialkylamino; R2 is H, alkyl, alkoxy, hydroxyalkylene, or halo; Z is NH, N-alkyl, or O; R5 is pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, quinazolinyl, quinoxalinyl, pyrazolyl, benzoxazolyl, imidazopyrazinyl, or triazolopyrazinyl, optionally substituted with a one or two substituents independently selected from the group consisting of alkyl, alkoxy, or halo; and n is 0 or 1. Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I.

Abstract: The present invention provides compounds useful as inhibitors of Btk, compositions thereof, and methods of using the same.

Abstract: Disclosed herein is novel highly stable, crystalline porphyrin containing covalent organic frameworks and their synthesis using Schiff base reaction which are hydrophobic in nature having good selectivity towards alcohol uptake at low pressure over water. Particularly, present invention provides novel highly stable, porous covalent organic frameworks (COFs) comprising porphyrin linked hydroxyl aromatic compound by intramolecular O—H—N?C bonding; wherein porphyrin is tetra(p-amino-phenyl)porphyrin (Tph) and hydroxyl aromatic compound is selected from group consisting of Triformylphloroglucinol (Tp), 2,5-dihydroxyterephthalaldehyde (Da).

Abstract: The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as TBK/IKK? inhibitors.

Abstract: The present invention provides a method for the preparation of orally available pentacyclic taxane compounds, as well as intermediates useful in their preparation.

Abstract: A method for producing a carboxylic acid anhydride includes heating a composition containing a specific compound in a solvent to yield the carboxylic acid anhydride. The solvent is an aprotic polar solvent having a boiling point of 50° C. or more.

Abstract: The present invention relates to a compound having the general formula II, optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which is useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.

Abstract: Provided are a series of novel pyridine or pyrimidine derivatives which inhibit CDK9 and may be useful for the treatment of hyperproliferative diseases. In particular the compounds are of use in the treatment of proliferative disease such as cancer including hematological malignancies such as acute myeloid leukemia, multiple myeloma, chronic lymphocytic leukemia, diffuse large B cell lymphoma, Burkitt's lymphoma, follicular lymphoma and solid tumors such as breast cancer, lung cancer, neuroblastoma and colon cancer.

Abstract: Macrocyclic benzodiazepine dimers having a structure represented by formula I where A and B are independently according to formulae Ia or Ib and the other variables in formulae I, Ia, and Ib are as defined in the application. Such dimers are useful as anti-cancer agents, especially when used as the drug component in an antibody-drug conjugate (ADC).

Abstract: The present invention provides a novel bicyclic or tricyclic heterocyclic compound represented by the formula (I) wherein ring A is an optionally substituted aromatic group, one of X1 and X2 is a carbon atom, and the other is a nitrogen atom, X3 is a nitrogen atom, or CR2, X4 is a nitrogen atom, or CR3, X5 is a sulfur atom, or —CH?CH—, Z1 is an oxygen atom, —C(R6)(R7)—, —NH—, —C(R6)(R7)—NH—, —NH—C(R6)(R7)—, —C(R6)(R7)—O—, —O—C(R6)(R7)—, or a single bond, one of Z2 and Z3 is CH and the other is a nitrogen atom, or both are nitrogen atoms, and other symbols are as defined in the DESCRIPTION, or a pharmacologically acceptable salt thereof.

Abstract: A series of substituted imidazo[2,1-b]thiazole derivatives, and analogues thereof, being potent modulators of human TNF? activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.

Abstract: Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.

Abstract: Described are methods of forming protected boronic acids that provide in a manner that is straightforward, scalable, and cost-effective a wide variety of building blocks, such as building blocks containing complex and/or pharmaceutically important structures, and/or provide simple or complex protected organoboronic acid building blocks. A first method includes reacting an imino-di-carboxylic acid and an organoboronate salt. A second method includes reacting a N-substituted morpholine dione and an organoboronic acid.

Abstract: Described herein are nickel pre-catalysts and related compositions and methods. The nickel pre-catalysts may be activated to form catalysts which may be utilized in organic reactions.

Abstract: In general, the invention features compounds useful for the synthesis of analogs of halichondrin B, such as eribulin or pharmaceutically acceptable salts thereof, e.g., eribulin mesylate.

Abstract: The invention relates to prodrug compounds of formula I: wherein R2, R3, R5, R7 and X are as defined herein. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including pain. The compounds of formula I possess advantageous solubility and physicochemical properties.

Abstract: Flavonoid compounds may be prepared that are selective for certain cell organelles, and may be used as biological imaging agents. Organelles that may be imaged with flavonoid compounds include mitochondria and lysosomes. Advantageously, the flavonoids show specificity to certain organelles and may exhibit a florescence “turn-on” mechanism, where the flavonoids that have target an organelle exhibit a florescence response when excited.

Abstract: The invention features compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.

Abstract: The present invention relates to a theranostic system comprising a beacon and a compound selected from the group consisting of a quinazoline-based tyrosine kinase inhibitor and a natural product. The theranostic systems have use in the therapy and diagnosis of tyrosine kinase related malignancies.

Abstract: The present invention is directed to a novel complex synthesized from a Salen-type ligand. The novel complex contains a quaternary ammonium salt. The present invention is also directed to a preparation method of a copolymer of carbon dioxide and epoxide using the complex synthesized from a Salen-type ligand as a catalyst.

Abstract: A method for depolymerization of lignin includes oxidizing non-phenolic lignin by putting into presence, in at least one solvent, non-phenolic lignin, laccase, redox mediator and a source of oxygen, whereby a mixture including oxidized non-phenolic lignin is obtained, and further includes depolymerization of the oxidized non-phenolic lignin thereby obtained, by adding an oxidizer. The non-phenolic lignin is obtained from phenolic lignin by functionalization of phenol functions of the phenolic lignin.

Abstract: The invention provides a method for releasing capsular polysaccharide from S. aureus type 5 or type 8 cells, comprising the step of treating the cells with acid. The invention further provides a process for purifying capsular polysaccharide from S. aureus type 5 or type 8 cells comprising this method. Other processing steps may be included in the process, such as enzymatic treatment, e.g. to remove nucleic acid, protein and/or peptidoglycan contaminants; diafiltration, e.g. to remove low molecular weight contaminants; anion exchange chromatography, e.g. to remove residual protein; and concentration.

Abstract: The present invention provides N-alkyl 2-(disubstituted)alkynyladenosine-5?-uronamides and derivatives thereof and pharmaceutical compositions containing the same that are selective agonists of A2A adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.

Abstract: A novel glycyrrhetinic acid derivative. The glycyrrhetinic acid derivative is represented by the following general formula.

Abstract: The present invention is directed to methods comprising the use of hydroxyapatite chromatography to separate a bispecific antibody from a solution that also comprises one or more byproducts specific to bispecific antibody production. Byproducts specific to the production of bispecific antibodies (bispecific antibody specific byproducts, “BASB”) include fragments of the bispecific antibody and heavier molecular weight variants of the antibody, wherein the fragment and/or variant comprises an Fc domain but does not exhibit affinity for the two different epitopes and/or antigens as exhibited by the desired bispecific antibody. Thus, the methods of the present invention comprise the separation of a bispecific antibody from one or more of its BASB. The hydroxyapatite chromatography methods of the invention may be used alone or may be further combined with standard purification processes and unit operations as is known in the art to achieve any level of purity of bispecific antibody necessary, e.g.

Abstract: Provided herein are methods for the production of native and reconstituted hyaluronan (HA) complexes containing pentraxin-3 (PTX3) and heavy chain 1 (HC1) of inter alpha inhibitor (I?I). Compositions containing the complexes and therapeutic methods using the complexes are provided. Combinations and kits for use in practicing the methods also are provided.